INSOLUTION H-89 DIHYDROCHLORIDE - CALBIOCHEM

General description

A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (K_i = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (K_i = 28.3 µM), Ca²⁺/calmodulin-dependent protein kinase II (K_i = 29.7 µM), protein kinase C (K_i = 31.7 µM), casein kinase I (K_i = 38.3 µM), and Rho Kinase II (IC₅₀ = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs), such as GEFI or Epac (exchange protein directly activated by cAMP) and GEFII. Reported to induce neurite formation in NG 108-15 cells (~1 mM) by blocking the action of Rho kinase II.

A cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (K_i = 48 nM). Inhibits other kinases only at much higher concentrations: CaM kinase II (K_i = 29.7 µM), casein kinase I (K_i = 38.3 µM), myosin light chain kinase (K_i = 28.3 µM), protein kinase C (K_i = 31.7 µM), and ROCK-II (IC₅₀ = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs) such as GEFI, GEFII, or Epac (exchange protein directly activated by cAMP). Enhances radiation-induced apoptosis in the human cell line BM 13674. A 10 mM (1 mg/193 µl) solution of H-89, 2HCl (Cat. No. 371962) in DMSO is also available.

Biochem/physiol Actions

Primary Target
PKA

Target K_i: 48 nM for protein kinase A

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, store in the refrigerator (4°C). Stock solutions are stable for at up to 4 months at 4°C.

Other Notes

Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther.300, 1000.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Kawasaki, H., et al. 1998. Science 282, 2275.
de Rooij, J., et al. 1998. Nature 396, 474.
Findik, D., et al. 1995. J. Cell. Biochem.57, 12.
Geilen, C.C. 1992. FEBS Lett.309, 381.
Chijiwa, T., et al. 1990. J. Biol. Chem.265, 5267.
Combest, W.L., et al. 1988. J. Neurochem.51, 1581.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany